| Item |
Information |
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Drug Groups
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illicit; approved; investigational |
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Description
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Pregabalin is an anticonvulsant drug used for neuropathic pain, as an adjunct therapy for partial seizures, and in generalized anxiety disorder. It was designed as a more potent successor to gabapentin. Pregabalin is marketed by Pfizer under the trade name Lyrica. It is considered to have a dependence liability if misused, and is classified as a Schedule V drug in the U.S. [Wikipedia] |
| Indication |
For management of neuropathic pain associated with diabetic peripheral neuropathy and postherpetic neuralgia. |
| Pharmacology |
Pregabalin is a new anticonvulsant drug indicated as an add on therapy for partial onset seizures and for certain types of neuropathic pain. It was designed as a more potent successor to a related drug, gabapentin. Pregabalin binds to the alpha2-delta subunit of the voltage-gated calcium channel in the central nervous system. While pregabalin is a structural derivative of the inhibitory neurotransmitter gamma- aminobutyric acid (GABA), it does not bind directly to GABAA, GABAB, or benzodiazepine receptors, does not augment GABAA responses in cultured neurons, does not alter rat brain GABA concentration or have acute effects on GABA uptake or degradation. However, in cultured neurons prolonged application of pregabalin increases the density of GABA transporter protein and increases the rate of functional GABA transport. Pregabalin does not block sodium channels, is not active at opiate receptors, and does not alter cyclooxygenase enzyme activity. It is inactive at serotonin and dopamine receptors and does not inhibit dopamine, serotonin, or noradrenaline reuptake. |
| Affected Organisms |
| • |
Humans and other mammals |
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| Biotransformation |
Negligible |
| Absorption |
Well absorbed after oral administration. |
| Half Life |
~6 hours |
| Elimination |
Pregabalin is eliminated from the systemic circulation primarily by renal excretion as unchanged drug. |
| Distribution |
* 0.5 L/kg |
| Clearance |
* Renal cl=67.0 – 80.9 mL/min [young healthy subjects] |
| References |
| • |
: Schedules of controlled substances: placement of pregabalin into schedule V. Final rule. Fed Regist. 2005 Jul 28;70(144):43633-5.
[Pubmed]
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| External Links |
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